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Degarelix

CAS No. : 214766-78-6

產(chǎn)品活性：Degarelix is a competitive and reversible gonadotropin-releasing hormone receptor (GnRHR/LHRHR) antagonist. Degarelix can be used for prostate cancer research.

研究領(lǐng)域：GPCR/G Protein  |  Apoptosis

作用靶點(diǎn)：GnRH Receptor  |  Apoptosis

In Vitro: Degarelix shows only very weak histamine-releasing properties and the lowest capacity for histamine release among the antagonists of LHRH, including Cetrorelix (HY-P0009), Abarelix (HY-13534), and Ganirelix (HY-P1628).
Degarelix (1 nM-10 μM, 0-72 h) reduces cell viability in all prostate cell lines (WPE1-NA22, WPMY-1, BPH-1, VCaP cells), with the exception of the PC-3 cells.
Degarelix (10 μM, 0-72 h) exerts a direct effect on prostate cell growth through apoptosis.

In Vivo: Degarelix (0-10 μg/kg; s.c.; once) decreases plasma LH levels and plasma testosterone levels in a dose-dependent manner in castrated rats.
Degarelix is stable when incubated in microsomes and cryopreserved hepatocytes from animal liver tissue. In rat and dog, most of the degarelix dose is eliminated within 48 h via urine and feces in equal amounts (40–50% in each matrix), whereas in monkey the major route of excretion is fecal (50%) and renal (22%).

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